RAJIVGANDHIUNIVERSITY OF HEALTH SCIENCES

BANGALORE, KARNATAKA.

ANNEXURE II

PROFORMA FOR REGISTRATION OF SUBJECTS FOR

P.G.DISSERTATION

6.0 / BRIEF RESUME OF THE INTENDED WORK
6.1 / NEED FOR THE STUDY:-
Thienopyrimidines are an interesting group of compounds with a wide range of biological activities. The biological activity of the compounds that remains in literatures are anti-microbial,anti-inflammatory,anti cancer, anti-convulsant, anti-bacterial, anti-hypertensive, antiviral, neurotropic and analgesic activities.
Thienopyrimidines also preventcartilage destruction in articular disease and shows DHFR (dihydrofolate reductase) inhibitory, VEGFR 2 kinase activity.
In this project it is proposed to synthesize 4-substituted thienopyrimidines with the aim to improve its biological activity and hence better utility as adrug.
6.2 / REVIEW OF LITERATURE:-
Synthesis and neurotropic activity of a series of new Pyrano(4', 3’:4, 5) thieno(3, 2-e) imidazolidino-(2, 1-b) pyrimidines was reported 1.
Synthesis and Anti-convulsant activity of a series of new Pyrano (thiopyrano) (4', 3’:4, 5) thieno (2, 3-d) pyrimidines was reported2.
Synthesis of 2-, 3- and 6-substituted tetrahydrobenzo (b) thieno (2, 3-d) pyrimidine-4-ones and their anti-convulsant activities was reported3.
Synthesis of certain fused thienopyrimidines of biological interest was reported4.
Microwave assisted synthesis of Novel 5-substituted-2, 3-dihydroimidazo (1,2-c) thieno (3, 2-e) pyrimidines was reported5.
 Synthesis and binding properties of novel selective 5-HT3 receptor ligands was reported 6.
Cytotoxic effects of NSL-1406, new thieno pyrimidine derivatives on leukocytes and osteoclasts were reported7.
Microwave-assisted of 2-aminothiophene-3-carboxylic acid derivatives, 3H-thieno (2, 3-d) pyrimidine-4-one and 4-chloro thieno (2, 3-d) pyrimidine was reported8.
Thieno pyrimidine derivatives prevent cartilage destruction in articular disease was reported9.
MCI-225, A Novel Thienopyrimidine Analog, enhances attentional eye tracking in midpontine pretrigeminal preparation was reported10.
Synthesis, antimicrobial and antiviral evaluation of certain thienopyrimidine derivatives reported11.
Furo(3, 4-d) pyrimidine-2, 4-dione derivative with antihypertensive activity. Analogs of thieno pyrimidine-2, 4-diones were reported12.
Synthesis, analgesic, anti-inflammatory,ulcerogenic index and antibacterial activities of Novel 2-methylthio-3-substituted-5, 6, 7, 8-tetrahydrobenzo (b) thieno (2, 3-d) pyrimidine-4(3H)-ones was reported13.
Design and SAR of thienopyrimidine and thieno pyrimidine inhibitors or VEGFR-2 kinase activity was reported14.
Thienopyrimidine urease as Novel and potent multitargated receptor tyrosine kinase inhibitors was reported15.
Synthesis of some new bioactive 3-amino-2-mercapto-5, 6, 7, 8-tetrahydro (1) benzothieno(2, 3,-d) pyrimidine-4(3H)-one derivatives was reported16.
Synthesis of some Novel 2-mercapto-3-(substituted amino) -5, 6, 7, 8-tetrahydro-3H-benzo (4, 5) thieno (2, 3-d) pyrimidine-4-ones as analgesic and anti-inflammatory agents was reported17.
Synthesis and DHFR inhibitory activity of a series of 6-substituted-2,4-diaminothieno (2,3-d) pyrimidines was reported18.
Synthesis and biological evaluation of 3-subsitutued derivatives of 4-phenyl-2-thioxo-benzo (4,5)thieno (2,3-d) pyrimidine was reported19.
6.3:-OBJECTIVE OF STUDY:-
The objective of the study is to synthesize substituted thieno (2, 3-4) pyrimidines and screen them for biological activity, so as to obtain chemical moiety with better efficacy and potency.
7.0:- MATERIALS AND METHODS
7.1:- SOURCE OF DATA:-
Chemical abstract and other journals like European journals of medicinal chemistry, Indian journal of chemistry, Asian journal of chemistry, Indian Institute of Science. , Bioorganic and Medicinal Chemistry. Bioorganic and Medicinal Chemistry letters. Indian journal of Heterocyclic Chemistry.
7.2:- METHODS OF DATA COLLECTION:-
Chemicals and other reagents will be collected from standard companies. The compounds will be synthesized. The product will purified by standard protocols. The separated compounds shall be characterized by UV, IR, NMR and Mass Spectroscopy.
7.3:-DOES THE STUDIES REQUIRE ANY INVESTIGATION TO BE CONDUCTED ON PATIENTS OR ANIMALS?
No.
7.4:-HAS ETHICAL CLEARENCE BEEN OBTAINED FROM YOUR INSTITUTION IN CASE OF 7.3?
Not Applicable.
8.0 / REFERENCES:-
  1. A.Sh.Oganisyan,A.S.Noravyan, I.A.Dzhagatspanyan and A.G.Akopyan.Dec.2001;35:number35.
  2. A.Sh.Oganisyan, A.S. Noravyan, I.A.Dzhagatspanyan and A.G.Akopyan. March 2001; 35:number3.
  3. A.P.Mkrtchyan, S.G.Kazaryan, A.S. Noravyan, R.A. Akopyan, I.A. Dzhagatspanyan, N.E.Akopyan and L.G.Akopyan. Nov.1986; 20:Number11.
  4. Journal of Chinese chemical society ISSN 0094536, 2006; 53.
  5. M. Raghu Parasad, A. R. Rama Rao, P. Shanthan Rao, Kombu. Subramanian Rajan. March2001.Thieme.
  6. Modica M., Romeo G., Materia L., Russo F., Cagnotto A., Mennini T. et all. Bioorganic and medicinal chemistry. July2004;12(14):3891-901.
  7. Katada J., KyokoIijima, Muramastu M., Takami M. et all.Bioorganic and Med. Chem.Letters.1999; 9:797-802.
  8. Tetrahedron Letters.23 July2007; 48(30)5261-264.
  9. Panico A., Cardile V, Andrea Satagatiand Barbara Gantile.Dec.2001; 56(12):959-64.
  10. Eguchi j, Saito Y, Mitsuo Egawa, Ken-Ichi Saito and Kawamura H.Pharmacology Biochemistry and Behavior. Feb.1997; 56(2):229-34.
  11. MA El-Sherbeny, MBEl-Ashmawy,HI El-Subbagh, AA El-Emam and FA Badria.European Journal of Med.Chem.1995; 30(5):445-449.
  12. Jeffery B.Press, James J.McNally, Joan A. Keiser, Steve j. Offord, Laurance B. Katz, Giardino E., Robert Falcotico and Alfonso Jobia.European J. of Med.Chem.Nov-Dec.1989; 24(6):627-630.
  13. V. Alagarsamy, S.Meena, K.V. Ramseshu, V.R. Soloman,K.Thirumurugan, K. Dhanabal and M.Murugan.Eu. J. of Med.Chem.Nov.2006; 41(11):1293-1300.
  14. Michael J.Munchhof, Jean S.Beebe, Jeffery M.Casavant, Beth A.Copper, et all.Bioorganic and Med.Chem. Letters.Jan.2004; 14(1):21-24.
  15. Yuji Dai, Yan Guo, Robin R Frey, Zhiquin Ji, and their co-workers.Journal of Med.Chem. Sep.2002; 48(19):6066-83.
  16. B.V.Ashalatha, B.Narayana, K.K.Vijay Raj, N.Scheta Kumari.Eu. J. of Med.Chem.2007; 42:719-28.
  17. Alagarsamy V, Shankar D and Viswas Raja Solomon.
  18. Hui Li, Sherry F. Queener, Donkor. Eu. J. of Med. Chem. Jun 2003; 38(6): 605-11.
  19. S Vega, J Alonso, J A Diaz, F Junquera, C Perez, V Darias et.al. Eu. J. of Med.Chem. Apr 1991; 26(3): 323-29.

9.0 / SIGNATURE OF THE CANDIDATE
10.0 / REMARKS OF THE GUIDE / Recommended for Dissertation work.
11.0 / NAME AND DESIGNATION OF
11.1:- GUIDE / Dr. L.V.G. Nargund
Professor
Dept. of Pharmaceutical Chemistry
NargundCollege of Pharmacy,
Bangalore-560085.
11.2:- SIGNATURE
11.3:- CO-GUIDE / Mrs. C.D.Saraswathi
Asst. Professor
Dept. of Pharmacology and Toxicology
NargundCollege of Pharmacy,
Bangalore-560085.
11.4:- SIGNATURE
11.5:- HEAD OF THE DEPT / Dr. L.V.G. Nargund
Professor and Head
Dept. of Pharmaceutical Chemistry
NargundCollege of Pharmacy,
Bangalore-560085.
11.6:- SIGNATURE
12.0 / REMARKS OF THE PRINCIPAL / Forwarded and Recommended
for favorable Consideration.
12.1:- SIGNATURE

Dept. Of Pharmaceutical Chemistry, N.C.P., Banglore-85